NZ608442A - Crystalline forms of a factor xa inhibitor - Google Patents

Crystalline forms of a factor xa inhibitor

Info

Publication number
NZ608442A
NZ608442A NZ60844211A NZ60844211A NZ608442A NZ 608442 A NZ608442 A NZ 608442A NZ 60844211 A NZ60844211 A NZ 60844211A NZ 60844211 A NZ60844211 A NZ 60844211A NZ 608442 A NZ608442 A NZ 608442A
Authority
NZ
New Zealand
Prior art keywords
crystalline forms
inhibitor
factor
betrixaban
maleate
Prior art date
Application number
NZ60844211A
Inventor
Vincent R Capodanno
Liam Corcoran
Michael Mcnevin
Itzia Zoraida Arroyo
Robert M Wenslow
Richard G Ball
Eric L Margelefsky
Timothy K Maher
Anjali Pandey
Original Assignee
Portola Pharm Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Portola Pharm Inc filed Critical Portola Pharm Inc
Publication of NZ608442A publication Critical patent/NZ608442A/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Two crystalline forms, Form II and Form III, of a maleate salt of betrixaban are described. Form II is an anhydrate and Form III is a hemihydrate. Betrixaban maleate is an inhibitor of the serine protease Factor Xa. The crystalline forms are useful for the treatment of thrombosis or thrombotic diseases.
NZ60844211A 2010-09-01 2011-08-31 Crystalline forms of a factor xa inhibitor NZ608442A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US37933910P 2010-09-01 2010-09-01
US201161454396P 2011-03-18 2011-03-18
PCT/US2011/050057 WO2012031017A1 (en) 2010-09-01 2011-08-31 CRYSTALLINE FORMS OF A FACTOR Xa INHIBITOR

Publications (1)

Publication Number Publication Date
NZ608442A true NZ608442A (en) 2015-04-24

Family

ID=45773260

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ60844211A NZ608442A (en) 2010-09-01 2011-08-31 Crystalline forms of a factor xa inhibitor

Country Status (13)

Country Link
US (1) US8946269B2 (en)
EP (1) EP2611779B1 (en)
JP (4) JP2013536864A (en)
CN (1) CN103261161B (en)
AR (1) AR082804A1 (en)
AU (1) AU2011295909B2 (en)
CA (1) CA2810004C (en)
ES (1) ES2603084T3 (en)
IL (1) IL224698A (en)
NZ (1) NZ608442A (en)
PT (1) PT2611779T (en)
TW (1) TW201221128A (en)
WO (1) WO2012031017A1 (en)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8980876B2 (en) 2010-10-28 2015-03-17 The Procter & Gamble Company Inhibition of microbial growth by aconitase inhibition
US20150224091A1 (en) * 2011-08-31 2015-08-13 Portola Pharmaceuticals, Inc. Prevention and treatment of thrombosis in medically ill patients
TWI686904B (en) * 2012-03-16 2020-03-01 美商樂仕特拉公司 Method and system for a photonic interposer
US20140346397A1 (en) 2012-12-27 2014-11-27 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
US9200268B2 (en) 2012-12-27 2015-12-01 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
CN104693114B (en) * 2013-12-10 2019-08-16 四川海思科制药有限公司 A kind of improved preparation method of betrixaban
CN105085387A (en) * 2014-05-20 2015-11-25 四川海思科制药有限公司 Betrixaban salt, preparation method and application thereof
WO2017091757A1 (en) * 2015-11-24 2017-06-01 Portola Pharmaceuticals, Inc. Isotopically enriched betrixaban
CN106995405A (en) * 2016-01-25 2017-08-01 重庆医药工业研究院有限责任公司 A kind of betrixaban maleate amorphous article and preparation method thereof
EP3463352A4 (en) * 2016-06-02 2019-10-30 Dr. Reddy S Laboratories Limited Polymorphs of betrixaban & its maleate salt
EP3254674A1 (en) 2016-06-08 2017-12-13 Sandoz Ag Pharmaceutical compositions of betrixaban maleate
EP3293174A1 (en) 2016-09-09 2018-03-14 Sandoz Ag Crystalline salts of betrixaban
WO2018069936A1 (en) 2016-10-13 2018-04-19 Mylan Laboratories Limited Polymorphs and solid dispersion of betrixaban and methods for the preparation thereof
CN107382897B (en) * 2017-07-10 2021-05-04 浙江宏元药业股份有限公司 Intermediate of betrixaban and preparation method and application thereof
EP3510996A1 (en) * 2018-01-11 2019-07-17 Sandoz AG Pharmaceutical compositions of betrixaban
CN108570003A (en) * 2018-06-01 2018-09-25 浙江宏元药业股份有限公司 A kind of water of betrixaban maleate is amorphous and preparation method thereof
WO2020264076A1 (en) 2019-06-28 2020-12-30 The Procter & Gamble Company Light augmented treatment method

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9226238D0 (en) 1992-12-16 1993-02-10 Scherer Ltd R P Encapsulation apparatus and process
US6140351A (en) 1997-12-19 2000-10-31 Berlex Laboratories, Inc. Ortho-anthranilamide derivatives as anti-coagulants
US6844367B1 (en) 1999-09-17 2005-01-18 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
US20020048610A1 (en) * 2000-01-07 2002-04-25 Cima Michael J. High-throughput formation, identification, and analysis of diverse solid-forms
US6376515B2 (en) 2000-02-29 2002-04-23 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor Xa
US6627646B2 (en) 2001-07-17 2003-09-30 Sepracor Inc. Norastemizole polymorphs
DE10322469A1 (en) 2003-05-19 2004-12-16 Bayer Healthcare Ag Heterocyclic compounds
JP5020073B2 (en) 2004-06-18 2012-09-05 ミレニアム ファーマシューティカルズ インク． Factor Xa inhibitor
US7696352B2 (en) 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
JP5227178B2 (en) 2005-11-08 2013-07-03 ミレニアム ファーマシューティカルズ， インコーポレイテッド N- (5-Chloro-2-pyridinyl) -2-[[4-[(dimethylamino) iminomethyl] benzoyl] amino] -5-methoxy-benzamide, pharmaceutical salts and polymorphs of factor Xa inhibitors
AR060768A1 (en) 2006-05-05 2008-07-10 Millennium Pharm Inc IMIDAZOL COMPOUNDS REPLACED INHIBITORS OF FACTOR X, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND USES AS ANTITROMBOTIC AGENTS.
US20080051578A1 (en) 2006-08-24 2008-02-28 Georg Dahmann Substituted biaryls, process for their manufacture and use thereof as medicaments
EP2077995B1 (en) 2006-11-02 2012-02-08 Millennium Pharmaceuticals, Inc. Methods of synthesizing pharmaceutical salts of a factor xa inhibitor
PT2101760E (en) 2006-12-08 2013-05-07 Millennium Pharm Inc Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor
CA2674924A1 (en) 2007-01-05 2008-07-17 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
EP2591783A1 (en) 2007-04-13 2013-05-15 Millennium Pharmaceuticals, Inc. Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor
NZ599556A (en) 2007-05-02 2013-10-25 Portola Pharm Inc Combination therapy with a compound acting as a platelet adp receptor inhibitor
PL3078743T3 (en) 2007-09-28 2020-11-02 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same
JP5709316B2 (en) * 2008-11-14 2015-04-30 ポートラ ファーマシューティカルズ， インコーポレイテッド Methods for using antidotes in combination with antidotes for factor Xa inhibitors and blood coagulants
PT2513058T (en) * 2009-12-17 2017-01-26 Millennium Pharm Inc Methods of synthesizing factor xa inhibitors
AR082803A1 (en) 2010-09-01 2013-01-09 Portola Pharm Inc METHODS AND FORMULATIONS FOR THE TREATMENT OF THROMBOSIS WITH BETRIXABAN AND A GLICOPROTEIN P INHIBITOR

Also Published As

Publication number Publication date
TW201221128A (en) 2012-06-01
ES2603084T3 (en) 2017-02-23
JP2013536864A (en) 2013-09-26
AU2011295909A1 (en) 2013-04-04
JP2018024709A (en) 2018-02-15
CA2810004C (en) 2019-09-10
CA2810004A1 (en) 2012-03-08
WO2012031017A1 (en) 2012-03-08
JP2019135258A (en) 2019-08-15
IL224698A (en) 2017-01-31
EP2611779A1 (en) 2013-07-10
EP2611779B1 (en) 2016-08-10
CN103261161A (en) 2013-08-21
PT2611779T (en) 2016-11-21
US20120071519A1 (en) 2012-03-22
US8946269B2 (en) 2015-02-03
AU2011295909B2 (en) 2015-05-21
CN103261161B (en) 2016-04-27
AR082804A1 (en) 2013-01-09
JP2015232046A (en) 2015-12-24

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